CDK4/6 inhibitor PRT3645

{
  "id": "MLC-T-ONC-012463",
  "term": "CDK4/6 inhibitor PRT3645",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, brain-penetrant, selective inhibitor of cyclin-dependent kinase (CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon oral administration, CDK4/6 inhibitor PRT3645 selectively targets and inhibits the activity of CDK4 and CDK6, which inhibits the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase, prevents CDK-mediated G1-S-phase transition and leads to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of both cell cycle progression from the G1-phase into the S-phase and tumor cell proliferation. PRT3645 is able to penetrate the brain and could exert its activity against CNS metastases in tumors with CDK4/6 upregulation.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/cdk4-6-inhibitor-prt3645/"
}